A selective inhibitor of NUAK1 (IC50 = 100 nM); partially inhibits the phosphorylation of the NUAK1 substrate MYPT1 at Ser445; inhibits proliferation and migration of mouse embryonic fibroblasts and U2OS cells at 10 µM in cell-based assays

HTH-01-015 – 10 mg

Brand:
Cayman
CAS:
1613724-42-7
Storage:
-20
UN-No:
Non-Hazardous - /

NUAK1 (also known as AMPK-related kinase 5) and NUAK2 (also known as SNF1/AMPK-related kinase) are members of the AMP-activated protein kinase (AMPK) family of protein kinases that are activated by the liver kinase B1 tumor suppressor kinase. NUAK kinases are thought to have roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity, and axon branching. HTH-01-015 is a selective inhibitor of NUAK1 (IC50 = 100 nM) and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.{30771} At 10 µM, HTH-01-015 has been shown to partially inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445.{30771} When administered to mouse embryonic fibroblasts in vitro, 10 µM HTH-01-015 inhibits proliferation and migration in a wound-healing assay.{30771} It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.{30771}  

 

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Description

A selective inhibitor of NUAK1 (IC50 = 100 nM); partially inhibits the phosphorylation of the NUAK1 substrate MYPT1 at Ser445; inhibits proliferation and migration of mouse embryonic fibroblasts and U2OS cells at 10 µM in cell-based assays

Formal name: 5,​13-​dihydro-​4,​5,​13-​trimethyl-​2-​[[1-​(4-​piperidinyl)​-​1H-​pyrazol-​4-​yl]​amino]​-6H-​naphtho[2,​3-​e]​pyrimido[5,​4-​b]​[1,​4]​diazepin-​6-​one

Synonyms: 

Molecular weight: 468.6

CAS: 1613724-42-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CaMKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|Cell Signaling

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